Boronic acid thrombin inhibitors
AssigneeTrigen Limited
InventorShouming Wang
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AssigneeTrigen Limited
InventorShouming Wang
Estimating the term…
A thrombin inhibitor selected from boronic acids of formula (I), and salts, prodrugs and prodrug salts thereof: wherein X is H (to form NH2) or an amino-protecting group; aa1 is an amino acid residue having a side chain selected from formula (A) and (B)—(CO)a—(CH2)b-Dc-(CH2)d-E (A), —(CO)a—(CH2)b-Dc-Ce(E1)(E2)(E3) wherein E1, E2 and E3 are 5-6 membered saturated or unsaturated hydrocarbyl rings, or one of E1, E2 and E3 is hydrogen and the other two are a said hydrocarbyl ring, E, E1, E2 and E3 optionally being halogenated when saturated and mandatorily being halogenated when unsaturated, a particular halogen being fluorine; aa2 is a residue of an amino acid which binds to the thrombin S2 subsite; and R9 is a straight chain alkyl group interrupted by one or more ether linkages or R9 is —(CH2)mW and W is —OH or halogen.
A compound selected from boronic acids of formula (I), and pharmaceutically acceptable salts, prodrugs and pharmaceutically acceptable prodrug salts thereof:
(canceled)
A compound selected from boronic acids of formula (II), and pharmaceutically acceptable salts, prodrugs and prodrug salts thereof:
23-24. (canceled)
A medicament comprising a salt, sugar ester or other soluble derivative of a boronic acid which is a selective thrombin inhibitor and has a neutral aminoboronic acid residue capable of binding to the thrombin S1 subsite linked to a hydrophobic moiety capable of binding to the thrombin S2 and S3 subsites, the hydrophobic moiety comprising a fluorinated ring in its S3-binding part and the salt comprising a cation having a valency n and having an observed stoichiometry consistent with a notional stoichiometry (boronic acid:cation) of n:1.
Dependencies are inferred from the claim text.